Direct Compression Formulations Used to Produce Lactose Free Loratadine (10 mg) Tablets

Formulations and Tablet Properties

Ingredients – Formulation 1 Mg/Tablet Percent (w/w)
Loratadine USP [Tricon
Enterprises]
10.00 6.67
Pregelatinized Starch NF
[Starch 1500®, Colorcon]
69.63 46.42
Microcrystalline Cellulose NF
[Emcocel® 90M, JRS Pharma]
69.63 46.42
Colloidal Silicon Dioxide NF
[Cab-o-sil® M-5P, Cabot]
0.37 0.25
Magnesium Stearate NF
[Mallinckrodt]
0.37 0.25
Total 150.00 100.00
Tablet Properties
Compaction Force 15 kN

Tablet Properties

(Round 9/32” standard concave)
Formula 1
Weight 148 mg
Thickness 3.65 mm
Hardness 7.0 kp
Friability 0.05%
Ejection Force 55 N
Disintegration Time 10 min
Dissolution (2.8 min) 99% released

Process (Direct Compression)

(Twin-shell blender)
A multi-step blending process was used in order to ensure proper distribution of the active. Initially, half of the Starch
1500® was combined with the drug and colloidal silicon dioxide. This mixture was blended in a twin shell “V”
blender for 5 minutes. The mixture was then discharged and passed through a 40-mesh screen by hand. This step not
only breaks up the silicon dioxide but also helps to distribute the active. The screened mixture was returned to the
blender and the remainder of the Starch 1500® was added and blended for an additional 5 minutes. The MCC was
then added and blended for 10 minutes. The magnesium stearate was added last and blended for 5 minutes. The
magnesium stearate was passed through a 60-mesh screen prior to weighing. Tablets were compressed using an
instrumented (SMI) Piccola (Riva) 10-station, rotary tablet press at 20 RPM. Tablet properties, hard- ness, thickness,
and weight were measured on an Erweka Multicheck. Friability was performed at 100 drops and disintegration times
were measured in DI water. Dissolution was tested in accordance with USP 28 in 0.1N HCl.
Formulation
Direct Compression
Loratadine 10 mg Tablets
Conclusion
Starch 1500® produced tablets with excellent hardness and friability values without the use of lactose as a
diluent. The formulation exhibited low ejection forces while using low levels of lubricants, thereby
reducing stress and wear on tooling and machinery. The use of Starch 1500® was also responsible for the
rapid disintegration of the tablets. These results show the strong disintegration functionality of Starch 1500®.
In addition to these benefits, a formulation containing Starch 1500® and microcrystalline cellulose rather than
lactose would show improved physical stability, as described in Colorcon Technical Data Sheet –
Lactose Replacement with Starch 1500® in a Direct Compression Formulation.